Department of Pharmacy, The Affiliated Hospital of Shandong University of Traditional Chinese Medicine, Jinan, China.
Department of Pharmacy, The Affiliated Hospital of Shandong University of Traditional Chinese Medicine, Jinan, China;, Email:
Pharmazie. 2021 Dec 5;76(12):568-573. doi: 10.1691/ph.2021.1820.
The PI3K/Akt/mTOR signaling pathway has the functions of regulating cell cycle, participating in tumor angiogenesis, affecting tumor invasion activity and metastasis, regulating apoptosis and autophagy, and participating in tumor drug resistance. Alpelisib (a PI3K inhibitor) has now been approved by the FDA for the treatment of PIK3CA mutant HR-positive/HER2-negative advanced/metastatic breast cancer in combination with fulvestrant which is the first PI3K inhibitor approved for breast cancer treatment. In some human colorectal cancer cells, the activation of this signal pathway is excessive and the negative regulation is impaired. Inhibitors targeting PI3K, a key protein in the PI3K/Akt/mTOR signaling pathway, have a positive effect on the treatment of colorectal cancer. Based on the role of PI3K/Akt/mTOR in the occurrence and development of colorectal cancer and its clinical application, this article reviews the PI3K inhibitors that have been on the market or are in clinical trials.
PI3K/Akt/mTOR 信号通路具有调节细胞周期、参与肿瘤血管生成、影响肿瘤侵袭活性和转移、调节细胞凋亡和自噬以及参与肿瘤耐药等功能。Alpelisib(一种 PI3K 抑制剂)已被 FDA 批准与氟维司群联合用于治疗 PIK3CA 突变的 HR 阳性/HER2 阴性晚期/转移性乳腺癌,这是第一种被批准用于乳腺癌治疗的 PI3K 抑制剂。在一些人结直肠癌细胞中,该信号通路的激活过度,负调控受损。针对 PI3K/Akt/mTOR 信号通路中的关键蛋白 PI3K 的抑制剂对结直肠癌的治疗有积极作用。基于 PI3K/Akt/mTOR 在结直肠癌发生发展中的作用及其临床应用,本文综述了已上市或正在临床试验中的 PI3K 抑制剂。